Quipazine dimaleate
Based on 1 Customer Validation
Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research.
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- Pureté: 99.96%
- CAS No.: 150323-78-7
- Formule: C21H23N3O8
- Masse moléculaire:445.42
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-HT3 Receptor |
Quipazine dimaleate shows binding efficacy to 5-HT1 and 5-HT2 with Ki values of 230 nM[3]. Quipazine dimaleate displaces [3H]GR65630 from 5-HT3R in rat entorhinal cortex with a Ki value of 1.4 nM[3]. Quipazine dimaleate shows antagonistic properties on the rat vagus nerve with pIC50 value of 6.1, 6.49 and 6.17 for 5-HT2, 5-HT1 and inhibition of 5-HT release[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female Wistar rats feed with different sources of the three macronutrients (Group 1: casein, corn starch, safflower oil. Group 2: egg protein, corn starch/sucrose, lard. Group S: casein hydrolysate, maltose dextrin, butter.)[1]
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Dosage:2.5, 5 and 7.5 mg/kg
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Administration:Intraperitoneal injection; 2.5, 5 and 7.5 mg/kg, one dose for once
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Result:Increased water intake and food intake of male rats from Group S, and reduced food intake of female rats from Group 1 and Group 2s at 2h post-injection. Reduced food intake in female rats from Group 2, reduced protein intake in female rats from Group 1.
Chemical Information
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CAS No. 150323-78-7
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Appearance Solid
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Masse moléculaire 445.42
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Formule C21H23N3O8
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Color White to off-white
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SMILES
O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.C1(N2CCNCC2)=NC3=CC=CC=C3C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 250 mg/mL (561.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Mok E, et al. Effect of quipazine, a selective 5-HT3 agonist, on dietary self-selection of different macronutrient diets in male and female rats. Appetite. 2000 Jun;34(3):313-25. [Content Brief]
[2]. Günther S, et al. X-ray screening identifies active site and allosteric inhibitors of SARS-CoV-2 main protease. Science. 2021 May 7;372(6542):642-646. [Content Brief]
[3]. Glennon RA, et al. 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80. [Content Brief]
[4]. Ireland SJ, Tyers MB. Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve. Br J Pharmacol. 1987 Jan;90(1):229-38. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2451 mL | 11.2254 mL | 22.4507 mL | 56.1268 mL |
| 5 mM | 0.4490 mL | 2.2451 mL | 4.4901 mL | 11.2254 mL | |
| 10 mM | 0.2245 mL | 1.1225 mL | 2.2451 mL | 5.6127 mL | |
| 15 mM | 0.1497 mL | 0.7484 mL | 1.4967 mL | 3.7418 mL | |
| 20 mM | 0.1123 mL | 0.5613 mL | 1.1225 mL | 2.8063 mL | |
| 25 mM | 0.0898 mL | 0.4490 mL | 0.8980 mL | 2.2451 mL | |
| 30 mM | 0.0748 mL | 0.3742 mL | 0.7484 mL | 1.8709 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5613 mL | 1.4032 mL | |
| 50 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1225 mL | |
| 60 mM | 0.0374 mL | 0.1871 mL | 0.3742 mL | 0.9354 mL | |
| 80 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7016 mL | |
| 100 mM | 0.0225 mL | 0.1123 mL | 0.2245 mL | 0.5613 mL |
Quipazine dimaleate Related Classifications
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